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A natural propenoic acid derivative activates peroxisome proliferator-activated receptor-beta/delta (PPARbeta/delta).

AbstractAIMS:
Previous studies showed that natural prenyloxyphenylpropanoid derivatives have potent biological properties in vivo. Given the structural similarities between these compounds and known peroxisome proliferator-activated receptor (PPAR) agonists, the present study examined the hypothesis that propenoic acid derivatives activate PPARs.
MAIN METHODS:
Chimeric reporter assays were performed to identify propenoic acid derivates that could activate PPARs. Quantitative polymerase chain reaction (qPCR) analysis of wild-type and Pparbeta/delta-null mouse primary keratinocytes was performed to determine if a test compound could specifically activate PPARbeta/delta. A human epithelial carcinoma cell line and primary mouse keratinocytes were used to determine the effect of the compound on cell proliferation.
KEY FINDINGS:
Three of the propenoic acid derivatives activated PPARs, with the greatest efficacy being observed with prenyloxycinnamic acid derivatives 4'-geranyloxyferulic acid (compound 1) for PPARbeta/delta. Compound 1 increased expression of a known PPARbeta/delta target gene through a mechanism that requires PPARbeta/delta. Inhibition of cell proliferation by compound 1 was found in a human epithelial carcinoma cell line.
SIGNIFICANCE:
Results from these studies demonstrate that compound 1 can activate PPARbeta/delta and inhibit cell proliferation of a human skin cancer cell line, suggesting that the biological effects of 4'-geranyloxyferulic acid may be mediated in part by activating this PPAR isoform.
AuthorsSalvatore Genovese, Jennifer E Foreman, Michael G Borland, Francesco Epifano, Frank J Gonzalez, Massimo Curini, Jeffrey M Peters
JournalLife sciences (Life Sci) Vol. 86 Issue 13-14 Pg. 493-8 (Mar 27 2010) ISSN: 1879-0631 [Electronic] Netherlands
PMID20153754 (Publication Type: Journal Article, Research Support, N.I.H., Extramural)
CopyrightCopyright 2010 Elsevier Inc. All rights reserved.
Chemical References
  • Coumarins
  • PPAR delta
  • PPAR-beta
  • Phenylpropionates
  • aurapten
Topics
  • Animals
  • COS Cells
  • Cell Line
  • Cell Line, Tumor
  • Cell Proliferation (drug effects)
  • Chlorocebus aethiops
  • Coumarins (chemistry, pharmacology)
  • Gene Expression Regulation (drug effects)
  • Humans
  • Mice
  • Molecular Structure
  • PPAR delta (metabolism)
  • PPAR-beta (metabolism)
  • Phenylpropionates (chemistry, pharmacology)
  • Polymerase Chain Reaction
  • Up-Regulation

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